A library of 54 ruthenium derivatives based on the trithiolato-bridged dinuclear ruthenium(II)-arene scaffold [(η⁶-arene)₂Ru₂(μ₂-SR¹)₂(μ₂-SR²)]⁺) was synthesized by introducing chemical modifications at the level of bridge thiols.
A three-step screening of the compounds was realized (i) activity against T. gondii and assessment of toxicity in non-infected HFF host cells; (ii) IC₅₀ measurements and (iii) studies on the effects in murine splenocytes.
The compound [(η⁶-p-MeC₆H₄Prⁱ)₂Ru₂(μ₂-SC₆H₄-o-CF₃)₂(μ₂-SC₆H₄-p-OH)]Cl exhibited the most favorable features.

This work was carried out in the group of Prof. Julien Furrer.

References:

• E. Paunescu, G. Boubaker, O. Desiatkina, N. Anghel, Y. Amdouni, A. Hemphill, J. Furrer;
  "The quest of the best - A SAR study of trithiolato-bridged dinuclear Ruthenium(II)-Arene compounds presenting antiparasitic properties"
  Eur. J. Med. Chem., 2021, 222, 113610/1-21; doi:10.1016/j.ejmech.2021.113610.